TAS1R1

Summary

TAS1R1 (taste 1 receptor member 1, HGNC:14448) is a protein-coding gene on chromosome 1p36.31, encoding Taste receptor type 1 member 1 (Q7RTX1). Putative taste receptor.

The protein encoded by this gene is a G protein-coupled receptor and is a component of the heterodimeric amino acid taste receptor T1R1+3. The T1R1+3 receptor responds to L-amino acids but not to D-enantiomers or other compounds. Most amino acids that are perceived as sweet activate T1R1+3, and this activation is strictly dependent on an intact T1R1+3 heterodimer. Multiple transcript variants encoding different isoforms have been found for this gene.

Source: NCBI Gene 80835 — RefSeq curated summary.

At a glance

• GWAS associations: 1
• Clinical variants (ClinVar): 121 total
• Druggable target: yes — 2 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_138697

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:14448
Approved symbol	TAS1R1
Name	taste 1 receptor member 1
Location	1p36.31
Locus type	gene with protein product
Status	Approved
Aliases	T1R1, TR1
Ensembl gene	ENSG00000173662
Ensembl biotype	protein_coding
OMIM	606225
Entrez	80835

Gene structure

Transcript identifiers

Ensembl transcripts: 4 — 4 protein_coding

ENST00000333172, ENST00000351136, ENST00000411823, ENST00000415267

RefSeq mRNA: 2 — MANE Select: NM_138697 NM_138697, NM_177540

CCDS: CCDS81, CCDS82

Canonical transcript exons

ENST00000333172 — 6 exons

Exon	Start	End
ENSE00001182045	6574631	6575392
ENSE00001182049	6576950	6577070
ENSE00001182053	6576415	6576627
ENSE00001182089	6570909	6571215
ENSE00001866244	6578653	6579755
ENSE00001879610	6555307	6555564

Expression profiles

Bgee: expression breadth ubiquitous, 116 present calls, max score 82.62.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.0982 / max 25.2756, expressed in 41 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter ID	TPM avg	Samples expressed
402	0.0410	14
401	0.0337	10
400	0.0235	8

Top tissues by expression

218 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	82.62	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	79.23	gold quality
left testis	UBERON:0004533	65.39	gold quality
right testis	UBERON:0004534	65.26	gold quality
testis	UBERON:0000473	63.38	gold quality
bone marrow cell	CL:0002092	60.11	gold quality
hindlimb stylopod muscle	UBERON:0004252	56.80	gold quality
endothelial cell	CL:0000115	56.65	gold quality
right adrenal gland cortex	UBERON:0035827	53.23	gold quality
gall bladder	UBERON:0002110	53.11	gold quality
gastrocnemius	UBERON:0001388	52.34	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	52.32	gold quality
parotid gland	UBERON:0001831	52.30	gold quality
muscle of leg	UBERON:0001383	52.26	gold quality
descending thoracic aorta	UBERON:0002345	51.57	gold quality
muscle layer of sigmoid colon	UBERON:0035805	51.08	gold quality
ascending aorta	UBERON:0001496	51.03	gold quality
skin of abdomen	UBERON:0001416	50.90	gold quality
thoracic aorta	UBERON:0001515	50.90	gold quality
spleen	UBERON:0002106	50.47	gold quality
right adrenal gland	UBERON:0001233	50.31	gold quality
adrenal cortex	UBERON:0001235	49.63	gold quality
left adrenal gland cortex	UBERON:0035825	49.59	gold quality
bone marrow	UBERON:0002371	49.31	silver quality
stromal cell of endometrium	CL:0002255	49.29	gold quality
aorta	UBERON:0000947	49.09	gold quality
left adrenal gland	UBERON:0001234	48.85	gold quality
granulocyte	CL:0000094	48.80	silver quality
right uterine tube	UBERON:0001302	48.30	gold quality
saliva-secreting gland	UBERON:0001044	48.22	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 0.

Experiment	Marker?	Max mean expression
E-ANND-3	no	2.26

Regulation

Is transcription factor: no

Literature-anchored findings (GeneRIF, showing 17)

• sequence differences in T1R receptors within and between species (human and mouse) can significantly influence the selectivity and specificity of taste responses (PMID:11894099)
• findings demonstrate the different functional roles of T1R3 and T1R2 and the presence of multiple ligand binding sites on the sweet taste receptor (PMID:15353592)
• In vivo taste bud signaling may proceed primarily through hT1R1 and hT1R2. (PMID:17506496)
• human duodenal L cells express sweet taste receptor T1r. (PMID:17724330)
• Taken together, these results suggest that Tas1R1-Tas1R3 receptor variants found in human fungiform papillae might contribute to inter-individual differences of sensitivity to L-glutamate. (PMID:19146926)
• In our sample of subjects, the frequencies of 2 nsSNPs, C329T in tas1r1 and C2269T in tas1r3, were significantly higher in [glutamate] nontasters than expected, whereas G1114A in tas1r1 was more frequent in tasters. (PMID:19571223)
• amino acid substitutions (A110V and R507Q) in the N-terminal ligand-binding domain of T1R1 severely impair receptor functions in vitro (PMID:21422378)
• Data show that that Tas1r1 and Tas1r3 are expressed in murine and human spermatozoa. (PMID:22427794)
• The study provides human psychophysical evidence that TAS1R1 polymorphisms associate with modest differences in overall taste intensity, which were independent from other well-studied markers of variation in oral sensation. (PMID:24000232)
• A complex molecular mechanism involving changes in the properties of both the orthosteric and non-orthosteric sites of T1R1 underlies the determination of ligand specificity in mammalian T1R1/T1R3. (PMID:24214976)
• Genetic variants in TAS1R were associated with dietary consumption, which may be associated with gastric cancer risk (PMID:27321875)
• Studied association of taste 1 receptor member 1 (TAS1R1) and taste 1 receptor member 3 (TAS1R3) single nucleotide polymorphisms (SNPs) with food choices at a buffet meal. and found certain TAS1R1 and TAS1R3 SNPs to be associated with fat and savoury-tasting and protein-rich food choices following a laboratory buffet in humans. (PMID:30518043)
• Using homology modeling, molecular docking and molecular dynamics (MD) simulations, this study investigates the effects of five natural umami ligands on the structural dynamics of T1R1-T1R3. (PMID:31092329)
• Oral Microbiota Profile Associates with Sugar Intake and Taste Preference Genes. (PMID:32138214)
• Association of taste receptor gene polymorphisms with dental caries. (PMID:32578798)
• Polymorphic variants in Sweet and Umami taste receptor genes and birthweight. (PMID:33654187)
• Gene expression analyses of TAS1R taste receptors relevant to the treatment of cardiometabolic disease. (PMID:37539767)

Cross-species orthologs

2 orthologs

Organism	Symbol	Gene ID
mus_musculus	Tas1r1	ENSMUSG00000028950
rattus_norvegicus	Tas1r1	ENSRNOG00000009708

Paralogs (4): CASR (ENSG00000036828), TAS1R3 (ENSG00000169962), GPRC6A (ENSG00000173612), TAS1R2 (ENSG00000179002)

Protein

Protein identifiers

Taste receptor type 1 member 1 — Q7RTX1 (reviewed: Q7RTX1)

Alternative names: G-protein coupled receptor 70

All UniProt accessions (3): Q7RTX1, H0Y6X0, H7C3W7

UniProt curated annotations — full annotation on UniProt →

Function. Putative taste receptor. TAS1R1/TAS1R3 responds to the umami taste stimulus (the taste of monosodium glutamate). Sequence differences within and between species can significantly influence the selectivity and specificity of taste responses.

Subunit / interactions. Forms heterodimers with TAS1R3.

Subcellular location. Cell membrane.

Miscellaneous. Incomplete sequence.

Similarity. Belongs to the G-protein coupled receptor 3 family. TAS1R subfamily.

Isoforms (4)

UniProt ID	Names	Canonical?
Q7RTX1-1	1, Gm148 form B	yes
Q7RTX1-2	2, Gm148 form C
Q7RTX1-3	3, Gm148 form A
Q7RTX1-4	4, Gm148 form D

RefSeq proteins (2): NP_619642, NP_803884 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000068	GPCR_3_Ca_sens_rcpt-rel	Family
IPR000337	GPCR_3	Family
IPR001828	ANF_lig-bd_rcpt	Domain
IPR011500	GPCR_3_9-Cys_dom	Domain
IPR017978	GPCR_3_C	Domain
IPR017979	GPCR_3_CS	Conserved_site
IPR028082	Peripla_BP_I	Homologous_superfamily
IPR038550	GPCR_3_9-Cys_sf	Homologous_superfamily

Pfam: PF00003, PF01094, PF07562

UniProt features (32 total): topological domain 8, transmembrane region 7, glycosylation site 6, splice variant 4, sequence variant 3, sequence conflict 2, signal peptide 1, chain 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q7RTX1-F1	88.29	0.62

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Glycosylation sites (6): 87, 88, 95, 291, 479, 529

Function

Pathways and Gene Ontology

Reactome pathways

3 pathways

ID	Pathway
R-HSA-418594	G alpha (i) signalling events
R-HSA-420499	Class C/3 (Metabotropic glutamate/pheromone receptors)
R-HSA-9717207	Sensory perception of sweet, bitter, and umami (glutamate) taste

MSigDB gene sets: 98 (showing top): MYOGENIN_Q6, GCANCTGNY_MYOD_Q6, GOBP_SENSORY_PERCEPTION_OF_CHEMICAL_STIMULUS, WHITE_NEUROBLASTOMA_WITH_1P36.3_DELETION, CAGCTG_AP4_Q5, AGCGCTT_MIR518F_MIR518E_MIR518A, CEBP_Q2, GOBP_DETECTION_OF_CHEMICAL_STIMULUS_INVOLVED_IN_SENSORY_PERCEPTION_OF_TASTE, AML_Q6, GOBP_SENSORY_PERCEPTION_OF_TASTE, ATGCTGG_MIR338, GOBP_DETECTION_OF_STIMULUS, GOBP_SENSORY_PERCEPTION, GOCC_PLASMA_MEMBRANE_SIGNALING_RECEPTOR_COMPLEX, GOCC_MEMBRANE_PROTEIN_COMPLEX

GO Biological Process (5): sensory perception of umami taste (GO:0050917), signal transduction (GO:0007165), G protein-coupled receptor signaling pathway (GO:0007186), sensory perception of taste (GO:0050909), detection of chemical stimulus involved in sensory perception of taste (GO:0050912)

GO Molecular Function (2): G protein-coupled receptor activity (GO:0004930), taste receptor activity (GO:0008527)

GO Cellular Component (2): plasma membrane (GO:0005886), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-3 pathways:

Category	Pathways
GPCR downstream signalling	1
GPCR ligand binding	1
Sensory perception of taste	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
sensory perception of taste	2
transmembrane signaling receptor activity	2
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
G protein-coupled receptor activity	1
signal transduction	1
sensory perception of chemical stimulus	1
detection of chemical stimulus involved in sensory perception	1
G protein-coupled receptor signaling pathway	1
detection of chemical stimulus involved in sensory perception of taste	1
membrane	1
cell periphery	1
cellular anatomical structure	1

Protein interactions and networks

STRING

1373 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
TAS1R1	TAS1R3	Q7RTX0	985
TAS1R1	GNAT3	A8MTJ3	960
TAS1R1	TAS1R2	Q8TE23	949
TAS1R1	TRPM5	Q9NZQ8	788
TAS1R1	SLC5A1	P13866	764
TAS1R1	GCG	P01275	749
TAS1R1	PLCB2	Q00722	735
TAS1R1	PKD2L1	Q9P0L9	719
TAS1R1	TAS2R38	P59533	713
TAS1R1	DVL1	O14640	680
TAS1R1	TAS2R16	Q9NYV7	667
TAS1R1	FFAR1	O14842	636
TAS1R1	PKD1L3	Q7Z443	632
TAS1R1	TAS2R1	Q9NYW7	621
TAS1R1	TAS2R41	P59536	618

IntAct

0 interactions, top by confidence:

BioGRID (4): TAS1R3 (Affinity Capture-Western), TAS1R1 (Negative Genetic), TAS1R1 (Affinity Capture-MS), TAS1R1 (Positive Genetic)

ESM2 similar proteins: A0A0G2K1Q8, A3QNZ8, A3QNZ9, A3QP00, A3QP01, A3QP07, A3QP08, A3QP09, D4A3T6, E1BPQ3, E9Q4J9, E9Q6I0, G5ECB2, O35659, O62714, O70410, O75899, O88871, P32082, P35384, P41180, P43220, P48442, P48960, Q49HI0, Q58Y75, Q5T6X5, Q5U9X3, Q61606, Q6TAC4, Q70VB1, Q717C1, Q7RTX1, Q80T41, Q8BG22, Q8K385, Q8K4Z6, Q8R420, Q8SQA4, Q8TE23

Diamond homologs: A3QNZ8, A3QNZ9, A3QP00, A3QP01, A3QP07, A3QP08, A3QP09, O62714, P35384, P41180, P48442, Q49HI0, Q7RTX1, Q8TE23, Q923K1, Q925I4, Q99PG6, Q9PW88, Q9QY96, Q9Z0R7, Q9Z0R8, Q49HH9, Q49KI5, E1BPQ3, E9Q6I0, O00222, O15303, O70410, P31421, P31422, P31423, P35349, P35400, P41594, P47743, P70579, Q14416, Q14831, Q14832, Q14833

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

121 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	92
Likely benign	10
Benign	4

Top pathogenic / likely-pathogenic (0)

SpliceAI

1075 predictions. Top by Δscore:

Variant	Effect	Δscore
1:6577066:GAGTG:G	donor_gain	1.0000
1:6577068:GTG:G	donor_gain	1.0000
1:6576413:A:AG	acceptor_gain	0.9900
1:6576414:G:GG	acceptor_gain	0.9900
1:6576414:GCTT:G	acceptor_gain	0.9900
1:6576580:C:G	donor_gain	0.9900
1:6576625:CAGGT:C	donor_loss	0.9900
1:6576626:AGGTA:A	donor_loss	0.9900
1:6576627:GG:G	donor_loss	0.9900
1:6576628:G:GC	donor_loss	0.9900
1:6571214:TGGT:T	donor_loss	0.9800
1:6571217:T:TT	donor_loss	0.9800
1:6574333:A:AG	acceptor_gain	0.9800
1:6575393:GT:G	donor_loss	0.9800
1:6575394:T:A	donor_loss	0.9800
1:6576414:GCT:G	acceptor_gain	0.9800
1:6576615:A:T	donor_gain	0.9800
1:6577069:TGG:T	donor_loss	0.9800
1:6577071:GT:G	donor_loss	0.9800
1:6577072:T:A	donor_loss	0.9800
1:6577073:GAG:G	donor_loss	0.9800
1:6577074:AG:A	donor_loss	0.9800
1:6571016:ACC:A	donor_gain	0.9700
1:6571020:GCT:G	donor_gain	0.9700
1:6571218:AA:A	donor_loss	0.9700
1:6574334:A:G	acceptor_gain	0.9700
1:6576414:GC:G	acceptor_gain	0.9700
1:6576944:TTACA:T	acceptor_loss	0.9700
1:6576945:TACAG:T	acceptor_loss	0.9700
1:6576946:ACAG:A	acceptor_loss	0.9700

AlphaMissense

5507 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
1:6579036:T:C	F660L	0.980
1:6579038:C:A	F660L	0.980
1:6579038:C:G	F660L	0.980
1:6579537:T:C	F827L	0.980
1:6579539:C:A	F827L	0.980
1:6579539:C:G	F827L	0.980
1:6574634:A:C	S168R	0.978
1:6574636:C:A	S168R	0.978
1:6574636:C:G	S168R	0.978
1:6578690:G:C	W544C	0.978
1:6578690:G:T	W544C	0.978
1:6579351:A:C	S765R	0.975
1:6579353:C:A	S765R	0.975
1:6579353:C:G	S765R	0.975
1:6579491:G:C	K811N	0.974
1:6579491:G:T	K811N	0.974
1:6577025:T:C	F517L	0.973
1:6577027:T:A	F517L	0.973
1:6577027:T:G	F517L	0.973
1:6579294:A:C	S746R	0.971
1:6579296:C:A	S746R	0.971
1:6579296:C:G	S746R	0.971
1:6574754:T:A	W208R	0.968
1:6574754:T:C	W208R	0.968
1:6579114:A:C	S686R	0.964
1:6579116:C:A	S686R	0.964
1:6579116:C:G	S686R	0.964
1:6579524:C:A	N822K	0.960
1:6579524:C:G	N822K	0.960
1:6577055:T:C	F527L	0.959

dbSNP variants (sampled 300 via entrez): RS1000024691 (1:6579158 G>A), RS1000068632 (1:6577753 G>A,T), RS1000080312 (1:6573764 G>A), RS1000269121 (1:6568380 G>A), RS1000368542 (1:6563047 C>A), RS1000403695 (1:6571883 C>T), RS1000440758 (1:6563365 C>G,T), RS1000565138 (1:6569404 C>T), RS1000599276 (1:6569588 C>T), RS1000705407 (1:6564307 C>A), RS1000768276 (1:6559189 G>A), RS1000841922 (1:6559396 G>A,C,T), RS1000853213 (1:6565952 C>A,G), RS1000885274 (1:6557795 C>T), RS1000997614 (1:6553836 T>C)

Disease associations

OMIM: gene MIM:606225 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

1 associations (top):

Study	Trait	p-value
GCST001134_1	White blood cell types	4.000000e-06

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0005090	basophil count

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL3832641 (PROTEIN COMPLEX)

Molecules with ChEMBL bioactivity

2 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 166,345 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL752	ADENOSINE PHOSPHATE	4	165,316
CHEMBL3715108	LACTISOLE SODIUM	1	1,029

PharmGKB: 1 entry (VIP=true, CPIC=false)

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: gpcr — Taste 1 receptors

Binding affinities (BindingDB)

157 measured of 160 human assays (160 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
N-hexan-3-yl-3-methyl-4-methylsulfanylbenzamide	EC50	120 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl 2-[(3-chloro-4-methoxybenzoyl)amino]hexanoate	EC50	120 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
N-hexan-3-yl-3,4-dimethylbenzamide	EC50	140 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl (2R)-2-[(4-ethenylbenzoyl)amino]-4-methylpentanoate	EC50	180 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
N’-[(2,4-dimethoxyphenyl)methyl]-N-[2-(furan-2-yl)ethyl]oxamide	EC50	180 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
N’-[(4-ethoxy-2-methoxyphenyl)methyl]-N-[2-(5-methyl-2-pyridinyl)ethyl]oxamide	EC50	190 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
4-methoxy-3-methyl-N-(2-methylpentan-3-yl)benzamide	EC50	200 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
4-methoxy-3-methyl-N-(2-methylhexan-3-yl)benzamide	EC50	200 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl (2R)-2-[(4-ethylsulfanylbenzoyl)amino]-4-methylpentanoate	EC50	200 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
3,6-dichloro-N-(4-ethoxyphenyl)-2-methoxybenzamide	EC50	220 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
N-heptan-4-yl-4-methoxy-3-methylbenzamide	EC50	220 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl (2R)-2-[(3,4-dimethylbenzoyl)amino]-3-methylbutanoate	EC50	250 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl (2R)-2-[(4-methoxy-3-methylbenzoyl)amino]-4-methylpentanoate	EC50	250 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
4-ethoxy-3-methyl-N-pentan-3-ylbenzamide	EC50	260 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
N-[(2R)-1-methoxy-4-methylpentan-2-yl]-3-methyl-4-methylsulfanylbenzamide	EC50	290 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
N-[(2,4-dimethoxyphenyl)methyl]-3-pyrrol-1-ylpyridine-4-carboxamide	EC50	290 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl 2-[(3-chloro-4-methoxybenzoyl)amino]pentanoate	EC50	290 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
(E)-N-(2,4-dimethylpentan-3-yl)-3-(4-methoxyphenyl)prop-2-enamide	EC50	290 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl (2S)-2-(1-benzofuran-2-carbonylamino)-4-methylpentanoate	EC50	310 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl (2S)-2-[(5-methoxy-1-benzofuran-2-carbonyl)amino]-4-methylpentanoate	EC50	320 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
4-ethoxy-N-heptan-4-ylbenzamide	EC50	320 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl (2R)-4-methyl-2-[(4-methylbenzoyl)amino]pentanoate	EC50	320 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl (2R)-2-[[(E)-3-(4-methoxyphenyl)prop-2-enoyl]amino]-4-methylpentanoate	EC50	320 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
3-(1,1-difluoroethyl)-N-heptan-4-ylbenzamide	EC50	330 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
N-heptan-4-yl-3-(trifluoromethyl)benzamide	EC50	330 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
4-ethyl-N-heptan-4-ylbenzamide	EC50	340 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
4-ethoxy-3-methyl-N-(5-methylhexan-3-yl)benzamide	EC50	340 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl (2R)-2-[(3-methoxy-4-methylbenzoyl)amino]-4-methylpentanoate	EC50	340 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl (2R,3R)-2-(1,3-benzodioxole-5-carbonylamino)-2,3-dimethylpentanoate	EC50	350 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
3-fluoro-N-heptan-4-yl-4-methoxybenzamide	EC50	350 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl (2R)-4-methyl-2-(naphthalene-2-carbonylamino)pentanoate	EC50	370 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
1-(2-chlorophenyl)-3-heptan-4-ylurea	EC50	370 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
2-methyl-N-(2-methylheptan-4-yl)-1,3-benzoxazole-5-carboxamide	EC50	380 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
N-heptan-4-yl-4-methylsulfanylbenzamide	EC50	390 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl (2S)-2-(1-benzothiophene-2-carbonylamino)-4-methylpentanoate	EC50	400 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
4-methoxy-3-methyl-N-(4-phenylbutan-2-yl)benzamide	EC50	400 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
3-chloro-4-methoxy-N-(2-methylcyclohexyl)benzamide	EC50	440 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
5-methoxy-N-[(2R)-1-methoxy-4-methylpentan-2-yl]-1-benzofuran-2-carboxamide	EC50	460 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
4-ethenyl-N-heptan-4-ylbenzamide	EC50	460 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
N-heptan-4-yl-4-methoxybenzamide	EC50	460 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
3-chloro-4-methoxy-N-pentan-2-ylbenzamide	EC50	470 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
5-bromo-N-heptan-4-ylfuran-2-carboxamide	EC50	490 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl 2-(1,3-benzodioxole-5-carbonylamino)hexanoate	EC50	490 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
1-(2,4-dichlorophenyl)-3-(1-phenylpropyl)urea	EC50	490 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
5-methyl-N-(5-methylhexan-3-yl)-1-benzofuran-2-carboxamide	EC50	500 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
N-hexan-3-yl-4-methyl-3-methylsulfanylbenzamide	EC50	500 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl (2R)-4-methyl-2-[(4-propoxybenzoyl)amino]pentanoate	EC50	510 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
N-heptan-4-yl-3-methylbenzamide	EC50	520 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
1-(2-chlorophenyl)-3-(2-methylcyclohexyl)urea	EC50	520 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators
methyl (2S)-2-(1H-indole-2-carbonylamino)-4-methylpentanoate	EC50	530 nM	US-9459250: Use of T1R3 venus flytrap region polypeptide to screen for taste modulators

ChEMBL bioactivities

411 potent at pChembl≥5 of 438 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
6.92	EC50	120	nM	CHEMBL3719142
6.92	EC50	120	nM	CHEMBL3717666
6.85	EC50	140	nM	CHEMBL3716217
6.85	EC50	140	nM	CHEMBL3717758
6.75	EC50	180	nM	CHEMBL3717202
6.75	EC50	180	nM	CHEMBL3715156
6.72	EC50	190	nM	CHEMBL3718834
6.72	IC50	190	nM	LACTISOLE SODIUM
6.72	EC50	190	nM	CHEMBL3719110
6.70	EC50	200	nM	CHEMBL3718431
6.70	EC50	200	nM	CHEMBL3719352
6.70	EC50	200	nM	CHEMBL3719220
6.68	IC50	210	nM	LACTISOLE SODIUM
6.68	EC50	210	nM	CHEMBL3716208
6.66	EC50	220	nM	CHEMBL3718284
6.66	EC50	220	nM	CHEMBL3714931
6.60	EC50	250	nM	CHEMBL3718656
6.60	EC50	250	nM	CHEMBL3715023
6.58	EC50	260	nM	CHEMBL3715281
6.54	EC50	290	nM	CHEMBL3717168
6.54	EC50	290	nM	CHEMBL3717504
6.54	EC50	290	nM	CHEMBL3717894
6.54	EC50	290	nM	CHEMBL3716393
6.51	EC50	310	nM	CHEMBL3715808
6.51	EC50	310	nM	CHEMBL4111248
6.50	EC50	320	nM	CHEMBL3718018
6.50	EC50	320	nM	CHEMBL3717726
6.50	EC50	320	nM	CHEMBL3715084
6.50	EC50	320	nM	CHEMBL3716141
6.50	EC50	320	nM	CHEMBL4114892
6.48	EC50	330	nM	CHEMBL3716606
6.48	EC50	330	nM	CHEMBL3909427
6.47	EC50	340	nM	CHEMBL3717635
6.47	EC50	340	nM	CHEMBL3719291
6.47	EC50	340	nM	CHEMBL3718505
6.46	EC50	350	nM	CHEMBL3717722
6.46	EC50	350	nM	CHEMBL3718486
6.46	IC50	350	nM	LACTISOLE SODIUM
6.46	EC50	350	nM	CHEMBL4107128
6.43	EC50	370	nM	CHEMBL3715936
6.43	EC50	370	nM	CHEMBL3715875
6.42	EC50	380	nM	CHEMBL3717692
6.41	EC50	390	nM	CHEMBL3715364
6.40	EC50	400	nM	CHEMBL3715954
6.40	EC50	400	nM	CHEMBL3717599
6.40	EC50	400	nM	CHEMBL4114511
6.38	EC50	420	nM	CHEMBL3715898
6.36	EC50	440	nM	CHEMBL3716867
6.35	EC50	450	nM	CHEMBL3717965
6.34	EC50	460	nM	CHEMBL3716609

CTD chemical–gene interactions

20 total (human), top 20 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
perfluorooctanoic acid	affects cotreatment, decreases expression	2
Estradiol	increases expression, affects expression, increases reaction, affects binding	2
tris(1,3-dichloro-2-propyl)phosphate	decreases expression	1
perfluorooctane sulfonic acid	affects cotreatment, decreases expression	1
perfluorohexanesulfonic acid	affects cotreatment, decreases expression	1
lactisole	affects binding, decreases activity	1
licochalcone B	increases expression	1
incobotulinumtoxinA	decreases expression	1
Resveratrol	decreases expression, affects cotreatment	1
Arsenic	affects methylation	1
Aspartame	affects reaction, affects binding, increases reaction, increases expression, affects localization	1
Benzo(a)pyrene	increases methylation	1
Glucose	affects binding, increases reaction, affects reaction, decreases expression	1
Plant Extracts	affects cotreatment, decreases expression	1
Sodium Glutamate	increases expression	1
Thiram	increases expression	1
Tobacco Smoke Pollution	decreases expression	1
Valproic Acid	increases methylation	1
Asbestos, Crocidolite	affects expression	1
Okadaic Acid	decreases expression	1

ChEMBL screening assays

37 unique, capped per target: 28 binding, 9 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL3720853	Binding	Activity at human T1R1/T1R3 expressed in HEK293T cells co-expressing Galpha15 assessed as induction of left-ward shift of glutamate dose response curve at 1 mM relative to untreated control	T1R hetero-oligomeric taste receptors, cell lines that express said receptors, and taste compounds
CHEMBL3720883	Functional	Inhibition of human T1R1/T1R3 expressed in HEK293T cells co-expressing Galpha15 assessed as calcium response by fluo-4-AM dye based FLIPR assay	T1R hetero-oligomeric taste receptors, cell lines that express said receptors, and taste compounds

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.